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Comparative neuropharmacology of three psychostimulant cathinone derivatives: butylone, mephedrone and methylone.(Report)

To purchase or authenticate to the full-text of this article, please visit this link: http://onlinelibrary.wiley.com/doi/10.1111/j.1476-5381.2012.01998.x/abstract Byline: Raul Lopez-Arnau(1), Jose Martinez-Clemente(1), David Pubill(1), Elena Escubedo(1)(*), Jorge Camarasa(1)(*) Keywords: butylone; m... Full description

Journal Title: British Journal of Pharmacology Sept, 2012, Vol.167, p.407(14)
Main Author: Lopez - Arnau, Raul
Other Authors: Martinez - Clemente, Jose , Pubill, David , Escubedo, Elena , Camarasa, Jorge
Format: Electronic Article Electronic Article
Language: English
Subjects:
Quelle: Cengage Learning, Inc.
ID: ISSN: 0007-1188
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title: Comparative neuropharmacology of three psychostimulant cathinone derivatives: butylone, mephedrone and methylone.(Report)
format: Article
creator:
  • Lopez - Arnau, Raul
  • Martinez - Clemente, Jose
  • Pubill, David
  • Escubedo, Elena
  • Camarasa, Jorge
subjects:
  • Norepinephrine
  • Dopamine Receptors
  • Haloperidol
  • Ecstasy (Drug)
ispartof: British Journal of Pharmacology, Sept, 2012, Vol.167, p.407(14)
description: To purchase or authenticate to the full-text of this article, please visit this link: http://onlinelibrary.wiley.com/doi/10.1111/j.1476-5381.2012.01998.x/abstract Byline: Raul Lopez-Arnau(1), Jose Martinez-Clemente(1), David Pubill(1), Elena Escubedo(1)(*), Jorge Camarasa(1)(*) Keywords: butylone; mephedrone; methylone; dopamine; serotonin; locomotor activity BACKGROUND AND PURPOSE Here, we have compared the neurochemical profile of three new cathinones, butylone, mephedrone and methylone, in terms of their potential to inhibit plasmalemmal and vesicular monoamine transporters. Their interaction with 5-HT and dopamine receptors and their psychostimulant effect was also studied. EXPERIMENTAL APPROACH Locomotor activity was recorded in mice following different doses of cathinones. Monoamine uptake assays were performed in purified rat synaptosomes. Radioligand-binding assays were carried out to assess the affinity of these compounds for monoamine transporters or receptors. KEY RESULTS Butylone, mephedrone and methylone (5-25 mgaekg.sub.-1) caused hyperlocomotion, which was prevented with ketanserin or haloperidol. Methylone was the most potent compound inhibiting both [.sub.3H]5-HT and [.sub.3H]dopamine uptake with IC.sub.50 values that correlate with its affinity for dopamine and 5-HT transporter. Mephedrone was found to be the cathinone derivative with highest affinity for vesicular monoamine transporter-2 causing the inhibition of dopamine uptake. The affinity of cathinones for 5-HT.sub.2A receptors was similar to that of MDMA. CONCLUSIONS AND IMPLICATIONS Butylone and methylone induced hyperlocomotion through activating 5-HT.sub.2A receptors and increasing extra-cellular dopamine. They inhibited 5-HT and dopamine uptake by competing with substrate. Methylone was the most potent 5-HT and dopamine uptake inhibitor and its effect partly persisted after withdrawal. Mephedrone-induced hyperlocomotion was dependent on endogenous 5-HT. Vesicular content played a key role in the effect of mephedrone, especially for 5-HT uptake inhibition. The potency of mephedrone in inhibiting noradrenaline uptake suggests a sympathetic effect of this cathinone. Author Affiliation: (1)Department of Pharmacology and Therapeutic Chemistry (Pharmacology Section) and Institute of Biomedicine (IBUB), University of Barcelona, Barcelona, Spain Correspondence: (*) Elena Escubedo, Department of Pharmacology and Therapeutic Chemistry, School of Pharmacy, University of Barcelona., Avda. J
language: English
source: Cengage Learning, Inc.
identifier: ISSN: 0007-1188
fulltext: fulltext
issn:
  • 0007-1188
  • 00071188
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titleComparative neuropharmacology of three psychostimulant cathinone derivatives: butylone, mephedrone and methylone.(Report)
creatorLopez - Arnau, Raul ; Martinez - Clemente, Jose ; Pubill, David ; Escubedo, Elena ; Camarasa, Jorge
ispartofBritish Journal of Pharmacology, Sept, 2012, Vol.167, p.407(14)
identifierISSN: 0007-1188
subjectNorepinephrine ; Dopamine Receptors ; Haloperidol ; Ecstasy (Drug)
descriptionTo purchase or authenticate to the full-text of this article, please visit this link: http://onlinelibrary.wiley.com/doi/10.1111/j.1476-5381.2012.01998.x/abstract Byline: Raul Lopez-Arnau(1), Jose Martinez-Clemente(1), David Pubill(1), Elena Escubedo(1)(*), Jorge Camarasa(1)(*) Keywords: butylone; mephedrone; methylone; dopamine; serotonin; locomotor activity BACKGROUND AND PURPOSE Here, we have compared the neurochemical profile of three new cathinones, butylone, mephedrone and methylone, in terms of their potential to inhibit plasmalemmal and vesicular monoamine transporters. Their interaction with 5-HT and dopamine receptors and their psychostimulant effect was also studied. EXPERIMENTAL APPROACH Locomotor activity was recorded in mice following different doses of cathinones. Monoamine uptake assays were performed in purified rat synaptosomes. Radioligand-binding assays were carried out to assess the affinity of these compounds for monoamine transporters or receptors. KEY RESULTS Butylone, mephedrone and methylone (5-25 mgaekg.sub.-1) caused hyperlocomotion, which was prevented with ketanserin or haloperidol. Methylone was the most potent compound inhibiting both [.sub.3H]5-HT and [.sub.3H]dopamine uptake with IC.sub.50 values that correlate with its affinity for dopamine and 5-HT transporter. Mephedrone was found to be the cathinone derivative with highest affinity for vesicular monoamine transporter-2 causing the inhibition of dopamine uptake. The affinity of cathinones for 5-HT.sub.2A receptors was similar to that of MDMA. CONCLUSIONS AND IMPLICATIONS Butylone and methylone induced hyperlocomotion through activating 5-HT.sub.2A receptors and increasing extra-cellular dopamine. They inhibited 5-HT and dopamine uptake by competing with substrate. Methylone was the most potent 5-HT and dopamine uptake inhibitor and its effect partly persisted after withdrawal. Mephedrone-induced hyperlocomotion was dependent on endogenous 5-HT. Vesicular content played a key role in the effect of mephedrone, especially for 5-HT uptake inhibition. The potency of mephedrone in inhibiting noradrenaline uptake suggests a sympathetic effect of this cathinone. Author Affiliation: (1)Department of Pharmacology and Therapeutic Chemistry (Pharmacology Section) and Institute of Biomedicine (IBUB), University of Barcelona, Barcelona, Spain Correspondence: (*) Elena Escubedo, Department of Pharmacology and Therapeutic Chemistry, School of Pharmacy, University of Barcelona., Avda. Joan XXIII s/n, Barcelona 08028, Spain. E-mail: eescubedo@ub.edu Article Note: (*) Contributed equally to this work. Received; 17 November 2011; Revised; 21 March 2012; Accepted; 6 April 2012
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titleComparative neuropharmacology of three psychostimulant cathinone derivatives: butylone, mephedrone and methylone.(Report)
descriptionTo purchase or authenticate to the full-text of this article, please visit this link: http://onlinelibrary.wiley.com/doi/10.1111/j.1476-5381.2012.01998.x/abstract Byline: Raul Lopez-Arnau(1), Jose Martinez-Clemente(1), David Pubill(1), Elena Escubedo(1)(*), Jorge Camarasa(1)(*) Keywords: butylone; mephedrone; methylone; dopamine; serotonin; locomotor activity BACKGROUND AND PURPOSE Here, we have compared the neurochemical profile of three new cathinones, butylone, mephedrone and methylone, in terms of their potential to inhibit plasmalemmal and vesicular monoamine transporters. Their interaction with 5-HT and dopamine receptors and their psychostimulant effect was also studied. EXPERIMENTAL APPROACH Locomotor activity was recorded in mice following different doses of cathinones. Monoamine uptake assays were performed in purified rat synaptosomes. Radioligand-binding assays were carried out to assess the affinity of these compounds for monoamine transporters or receptors. KEY RESULTS Butylone, mephedrone and methylone (5-25 mgaekg.sub.-1) caused hyperlocomotion, which was prevented with ketanserin or haloperidol. Methylone was the most potent compound inhibiting both [.sub.3H]5-HT and [.sub.3H]dopamine uptake with IC.sub.50 values that correlate with its affinity for dopamine and 5-HT transporter. Mephedrone was found to be the cathinone derivative with highest affinity for vesicular monoamine transporter-2 causing the inhibition of dopamine uptake. The affinity of cathinones for 5-HT.sub.2A receptors was similar to that of MDMA. CONCLUSIONS AND IMPLICATIONS Butylone and methylone induced hyperlocomotion through activating 5-HT.sub.2A receptors and increasing extra-cellular dopamine. They inhibited 5-HT and dopamine uptake by competing with substrate. Methylone was the most potent 5-HT and dopamine uptake inhibitor and its effect partly persisted after withdrawal. Mephedrone-induced hyperlocomotion was dependent on endogenous 5-HT. Vesicular content played a key role in the effect of mephedrone, especially for 5-HT uptake inhibition. The potency of mephedrone in inhibiting noradrenaline uptake suggests a sympathetic effect of this cathinone. Author Affiliation: (1)Department of Pharmacology and Therapeutic Chemistry (Pharmacology Section) and Institute of Biomedicine (IBUB), University of Barcelona, Barcelona, Spain Correspondence: (*) Elena Escubedo, Department of Pharmacology and Therapeutic Chemistry, School of Pharmacy, University of Barcelona., Avda. Joan XXIII s/n, Barcelona 08028, Spain. E-mail: eescubedo@ub.edu Article Note: (*) Contributed equally to this work. Received; 17 November 2011; Revised; 21 March 2012; Accepted; 6 April 2012
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abstractTo purchase or authenticate to the full-text of this article, please visit this link: http://onlinelibrary.wiley.com/doi/10.1111/j.1476-5381.2012.01998.x/abstract Byline: Raul Lopez-Arnau(1), Jose Martinez-Clemente(1), David Pubill(1), Elena Escubedo(1)(*), Jorge Camarasa(1)(*) Keywords: butylone; mephedrone; methylone; dopamine; serotonin; locomotor activity BACKGROUND AND PURPOSE Here, we have compared the neurochemical profile of three new cathinones, butylone, mephedrone and methylone, in terms of their potential to inhibit plasmalemmal and vesicular monoamine transporters. Their interaction with 5-HT and dopamine receptors and their psychostimulant effect was also studied. EXPERIMENTAL APPROACH Locomotor activity was recorded in mice following different doses of cathinones. Monoamine uptake assays were performed in purified rat synaptosomes. Radioligand-binding assays were carried out to assess the affinity of these compounds for monoamine transporters or receptors. KEY RESULTS Butylone, mephedrone and methylone (5-25 mgaekg.sub.-1) caused hyperlocomotion, which was prevented with ketanserin or haloperidol. Methylone was the most potent compound inhibiting both [.sub.3H]5-HT and [.sub.3H]dopamine uptake with IC.sub.50 values that correlate with its affinity for dopamine and 5-HT transporter. Mephedrone was found to be the cathinone derivative with highest affinity for vesicular monoamine transporter-2 causing the inhibition of dopamine uptake. The affinity of cathinones for 5-HT.sub.2A receptors was similar to that of MDMA. CONCLUSIONS AND IMPLICATIONS Butylone and methylone induced hyperlocomotion through activating 5-HT.sub.2A receptors and increasing extra-cellular dopamine. They inhibited 5-HT and dopamine uptake by competing with substrate. Methylone was the most potent 5-HT and dopamine uptake inhibitor and its effect partly persisted after withdrawal. Mephedrone-induced hyperlocomotion was dependent on endogenous 5-HT. Vesicular content played a key role in the effect of mephedrone, especially for 5-HT uptake inhibition. The potency of mephedrone in inhibiting noradrenaline uptake suggests a sympathetic effect of this cathinone. Author Affiliation: (1)Department of Pharmacology and Therapeutic Chemistry (Pharmacology Section) and Institute of Biomedicine (IBUB), University of Barcelona, Barcelona, Spain Correspondence: (*) Elena Escubedo, Department of Pharmacology and Therapeutic Chemistry, School of Pharmacy, University of Barcelona., Avda. Joan XXIII s/n, Barcelona 08028, Spain. E-mail: eescubedo@ub.edu Article Note: (*) Contributed equally to this work. Received; 17 November 2011; Revised; 21 March 2012; Accepted; 6 April 2012
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